- Synthesis of novel 1,2,3-triazole derivatives of isocoumarins and 3,4-dihydroisocoumarin with potential antiplasmodial activity in vitro
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Background: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, dem-onstrating the need for the development of new antimalarial drugs. Objective: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocou-marins and a 3,4-dihydroisocoumarin. Methods: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an un-precedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). Results: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89 μM and 0.85-2.07 μM against W2 and 3D7 strains, respectively. Conclusion: This study demonstrated the great potential of isocoumarin or 3,4-dihydroisocoumarin derivatives because practically all the tested substances were active against Plasmodium falciparum.
- Alves, Rosemeire Brondi,Pinto, Ana Claudia de Souza,Santos, Lucas da Silva,Varotti, Fernando de Pilla,da Fonseca, Amanda Luisa,de Carvalho, Matheus Fillipe Langanke,de Freitas, Rossimiriam Pereira,Lopes, Julio César Dias
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p. 820 - 833
(2021/10/21)
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- NRF2 REGULATORS
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The present invention relates to aryl analogs Formula (I), pharmaceutical compositions containing them and their use as Nrf2 regulators.
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Page/Page column 52
(2017/01/02)
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- Synthesis and antiproliferative activity of 8-hydroxyquinoline derivatives containing a 1,2,3-triazole moiety
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Twelve novel 8-hydroxyquinoline derivatives were synthesized with good yields by performing coppercatalyzed Huisgen 1,3-dipolar cycloaddition ("click" reaction) between an 8-O-alkylated-quinoline containing a terminal alkyne and various aromatic or protected sugar azides. These compounds were evaluated in vitro for their antiproliferative activity on various cancer cell types. Protected sugar derivative 16 was the most active compound in the series, exhibiting potent antiproliferative activity and high selectivity toward ovarian cancer cells (OVCAR-03, GI50 -1); this derivative was more active than the reference drug doxorubicin (OVCAR-03, GI50 = 0.43 μg mL-1). In structureeactivity relationship (SAR) studies, the physico-chemical parameters of the compounds were evaluated and docking calculations were performed for the a-glucosidase active site to predict the possible mechanism of action of this series of compounds.
- De O. Freitas, Luiza B.,Borgati, Thiago F.,De Freitas, Rossimiriam P.,Ruiz, Ana L. T. G.,Marchetti, Gabriela M.,De Carvalho, Joo E.,Da Cunha, Elaine F. F.,Ramalho, Teodorico C.,Alves, Rosemeire B.
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p. 595 - 604
(2015/03/14)
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- Synthesis and phytotoxic activity of 1,2,3-triazole derivatives
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Thirteen triazole derivatives bearing halogenated benzyl substituents were synthesized using the Cu-catalyzed azide-alkyne cycloaddition (CuAAC),a leading example of the click chemistry approach,as the key step. The biological activity of the compounds was evaluated,and it was found that these compounds interfere with the germination and radicle growth (shoots and roots) of two dicotyledonous species,Lactuca sativa and Cucumis sativus,and one monocotyledonous species,Allium cepa. The compounds showed predominantly inhibitory activity related to the evaluated species mainly at the concentration of 10-4 mol L-1. Some of them presented inhibitory activity comparable to 2,4-D (2,4-dichlorophenoxyacetic acid),used as positive control.
- Borgati, Thiago F.,Alves, Rosemeire B.,Teixeira, Ro?bson R.,De Freitas, Rossimiriam P.,Perdiga?o, Thays G.,Da Silva, Silma F.,Dos Santos, Aline Aparecida,De Jesu?s O. Bastidas, Alberto
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p. 953 - 961
(2013/08/23)
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- SUBSTITUTED ISOXAZOLINE DERIVATIVES
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This invention recites substituted isoxazoline derivatives of Formula (1) or a veterinarily acceptable salt thereof, with parasiticidal activity, compositions thereof, and their use as a parasiticide in animals or birds where R1a, R1b/sup
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- HCV NS3 PROTEASE INHIBITORS
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The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
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Page/Page column 55-56
(2008/12/05)
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